(-)-Bicuculline methiodide

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CAS NO:

40709-69-1

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	Yellow solid
Storage	Store at RT
M.Wt	509.3
Cas No.	40709-69-1
Formula	C₂₁H₂₀INO₆
Solubility	<10.19mg/ml in H2O;<25.46mg/ml in DMSO
Chemical Name	(S)-6,6-dimethyl-5-((R)-8-oxo-6,8-dihydro-[1,3]dioxolo[4,5-e]isobenzofuran-6-yl)-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-6-ium iodide
Canonical SMILES	O=C1O[C@H](C(C=C2)=C1C3=C2OCO3)[C@H](C4=C5)[N+](C)(C)CCC4=CC6=C5OCO6.[I-]
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

(-)-Bicuculline methiodide is an antagonist of γ-aminobutyric acid-A (GABA_A) receptor, with IC50 value of 500 μM for GABA binding [1].

Three classes of GABA receptors have been characterized based on their pharmacology, namely GABA_A, GABA_B and GABA_C receptors, among which GABA_A and GABA_C receptors are ligand-gated chloride (Cl^-) channels. GABA receptors play important roles in central nervous system by responding to the inhibitory neurotransmitter GABA [2].

On synaptic membranes of chick cerebellum at birth, (-)-bicuculline methiodide acted as a less potent convulsant than (+)-Bicuculline methiodide which was more effective in displacing GABA binding, with an IC50 value of 10 μM [1]. InC. elegans, (-)-bicuculline methiodide at the concentration of 10 μM did not inhibit UNC-49B homomeric or UNC-49B/C heteromeric receptors which are UNC-49 subunits most closely related to the bicuculline- and benzodiazepine-insensitive RDL GABA receptors of insects. (-)-Bicuculline methiodide was used to confirm that the UNC-49 receptors were pharmacologically distinct from the mammalian GABA_A receptors [3].

References:

[1]. Fiszer De Plazas S. Ontogenesis of GABA receptor sites in chick embryo cerebellum. Brain Research, 1982, 255(2): 263-275.

[2]. Goutman J D, Calvo D J. Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor. British Journal of Pharmacology, 2004, 141(4): 717-727.

[3]. Bamber B A, Twyman R E, Jorgensen E M. Pharmacological characterization of the homomeric and heteromeric UNC-49 GABA receptors inC. elegans. British Journal of Pharmacology, 2003, 138(5): 883-893.